ECSP12012210A - HETEROARIL-CICLOHEXIL-TETRAAZABENZO [e] AZULENOS - Google Patents

HETEROARIL-CICLOHEXIL-TETRAAZABENZO [e] AZULENOS

Info

Publication number
ECSP12012210A
ECSP12012210A ECSP12012210A ECSP12012210A EC SP12012210 A ECSP12012210 A EC SP12012210A EC SP12012210 A ECSP12012210 A EC SP12012210A EC SP12012210 A ECSP12012210 A EC SP12012210A
Authority
EC
Ecuador
Prior art keywords
formula
tetraazabenzo
receptor
relates
present
Prior art date
Application number
Other languages
English (en)
Inventor
Patrick Schnider
Cosimo Dolente
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ECSP12012210A publication Critical patent/ECSP12012210A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

La presente invención se refiere a heteroaril-ciclo-hexil-tetraazabenzo[e]azulenos de la fórmula I (consta fórmula) en la que R1, R2 y R3 tienen los significados aquí descritos. Los compuestos de la invención actúan como moduladores del receptor de la V1a y en particular como antagonistas del receptor de la V1a; la invención se refiere además a su obtención, a las composiciones farmacéuticas que los contienen y al uso de los mismos como medicamentos. Los compuestos activos de la presente invención son útiles como agentes terapéuticos que actúan a nivel periférico y central en los estados patológicos tales como la dismenorrea, disfunción sexual masculina o femenina, hipertensión, fallo cardíaco crónico, secreción inapropiada de vasopresina, cirrosis hepática, síndrome nefrótico, ansiedad, trastornos depresivos, trastorno obsesivo-compulsivo, trastornos del espectro autista, esquizofrenia y conducta agresiva.
ECSP12012210 2010-04-21 2012-10-02 HETEROARIL-CICLOHEXIL-TETRAAZABENZO [e] AZULENOS ECSP12012210A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10160643 2010-04-21

Publications (1)

Publication Number Publication Date
ECSP12012210A true ECSP12012210A (es) 2012-10-30

Family

ID=43919925

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP12012210 ECSP12012210A (es) 2010-04-21 2012-10-02 HETEROARIL-CICLOHEXIL-TETRAAZABENZO [e] AZULENOS

Country Status (35)

Country Link
US (1) US8492376B2 (es)
EP (1) EP2560975B1 (es)
JP (1) JP5579923B2 (es)
KR (1) KR101506776B1 (es)
CN (1) CN102858776B (es)
AR (1) AR080927A1 (es)
AU (1) AU2011244407B2 (es)
BR (1) BR112012026890A2 (es)
CA (1) CA2795526A1 (es)
CL (1) CL2012002905A1 (es)
CO (1) CO6640209A2 (es)
CR (1) CR20120513A (es)
CY (1) CY1116661T1 (es)
DK (1) DK2560975T3 (es)
EA (1) EA021418B1 (es)
EC (1) ECSP12012210A (es)
ES (1) ES2542953T3 (es)
HR (1) HRP20150929T1 (es)
HU (1) HUE026538T2 (es)
IL (1) IL222403A (es)
MA (1) MA34174B1 (es)
MX (1) MX2012012046A (es)
MY (1) MY160457A (es)
NZ (1) NZ602627A (es)
PE (2) PE20130190A1 (es)
PH (1) PH12012502066A1 (es)
PL (1) PL2560975T3 (es)
PT (1) PT2560975E (es)
RS (1) RS54121B1 (es)
SG (1) SG184534A1 (es)
SI (1) SI2560975T1 (es)
TW (1) TWI419890B (es)
UA (1) UA109543C2 (es)
WO (1) WO2011131596A1 (es)
ZA (1) ZA201207689B (es)

Families Citing this family (17)

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AU2009315754B2 (en) * 2008-11-13 2013-08-15 F. Hoffmann-La Roche Ag Spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes
PE20110590A1 (es) * 2008-11-18 2011-08-31 Hoffmann La Roche Alquilciclohexileteres de dihidrotetraazabenzoazulenos
BRPI0922303B1 (pt) * 2008-11-28 2019-11-12 Hoffmann La Roche arilciclo-hexiléteres de di-hidrotetra-azabenzoazulenos, seu processo de preparação, composição farmacêutica que os compreende e uso
US8420633B2 (en) 2010-03-31 2013-04-16 Hoffmann-La Roche Inc. Aryl-cyclohexyl-tetraazabenzo[e]azulenes
US8461151B2 (en) 2010-04-13 2013-06-11 Hoffmann-La Roche Inc. Aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes
US8492376B2 (en) 2010-04-21 2013-07-23 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes
US8513238B2 (en) 2010-05-10 2013-08-20 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[E]azulenes
HRP20210966T1 (hr) 2013-12-05 2021-09-17 F. Hoffmann - La Roche Ag Sinteza trans-8-kloro-5-metil-1-[4-(piridin-2-iloksi)-cikloheksil]-5,6-dihidro-4h-2,3,5,10b-tetraaza­benzo[e]azulena i njegovih kristalnih oblika
WO2017191117A1 (en) 2016-05-03 2017-11-09 Bayer Pharma Aktiengesellschaft V1a receptor antagonists for use in the treatment of renal diseases
MX2020004105A (es) * 2017-12-08 2020-09-22 Hoffmann La Roche Formulacion farmaceutica.
TW201938171A (zh) * 2017-12-15 2019-10-01 匈牙利商羅特格登公司 作為血管升壓素V1a受體拮抗劑之三環化合物
HU231206B1 (hu) 2017-12-15 2021-10-28 Richter Gedeon Nyrt. Triazolobenzazepinek
EP3894414B1 (en) * 2018-12-12 2024-04-10 Neumora Therapeutics, Inc. 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives as vasopressin antagonists for the treatment of neuro-psychological disorders
WO2022018121A1 (en) * 2020-07-23 2022-01-27 F. Hoffmann-La Roche Ag Cyclohexyl substituted triazoles as vasopressin receptor v1 a antagonists
WO2022018105A1 (en) * 2020-07-23 2022-01-27 F. Hoffmann-La Roche Ag Heteroaryl-methyl substituted triazoles as vasopressin receptor v1 a antagonists
CN114644635B (zh) * 2020-12-21 2023-02-03 上海济煜医药科技有限公司 三氮唑类三并环衍生物及其制备方法和应用
CN116836111A (zh) * 2023-09-01 2023-10-03 峰成医药科技(天津)有限公司 一种氟代吡啶的连续化合成方法

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US8420633B2 (en) 2010-03-31 2013-04-16 Hoffmann-La Roche Inc. Aryl-cyclohexyl-tetraazabenzo[e]azulenes
US8461151B2 (en) 2010-04-13 2013-06-11 Hoffmann-La Roche Inc. Aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes
US8492376B2 (en) 2010-04-21 2013-07-23 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes
US8513238B2 (en) 2010-05-10 2013-08-20 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[E]azulenes

Also Published As

Publication number Publication date
MA34174B1 (fr) 2013-04-03
CO6640209A2 (es) 2013-03-22
CN102858776A (zh) 2013-01-02
PT2560975E (pt) 2015-08-28
AR080927A1 (es) 2012-05-16
NZ602627A (en) 2013-07-26
CA2795526A1 (en) 2011-10-27
MX2012012046A (es) 2012-11-22
AU2011244407A1 (en) 2012-10-18
BR112012026890A2 (pt) 2016-07-19
CL2012002905A1 (es) 2013-03-22
CY1116661T1 (el) 2017-03-15
ES2542953T3 (es) 2015-08-13
PE20160589A1 (es) 2016-06-11
TW201139444A (en) 2011-11-16
RS54121B1 (sr) 2015-12-31
SG184534A1 (en) 2012-11-29
WO2011131596A1 (en) 2011-10-27
AU2011244407B2 (en) 2013-06-13
TWI419890B (zh) 2013-12-21
EP2560975A1 (en) 2013-02-27
HK1176609A1 (zh) 2013-08-02
ZA201207689B (en) 2015-06-24
EA021418B1 (ru) 2015-06-30
MY160457A (en) 2017-03-15
EP2560975B1 (en) 2015-06-17
HUE026538T2 (en) 2016-06-28
US20110263578A1 (en) 2011-10-27
EA201291092A1 (ru) 2013-04-30
PE20130190A1 (es) 2013-02-21
JP5579923B2 (ja) 2014-08-27
HRP20150929T1 (hr) 2015-10-09
JP2013525319A (ja) 2013-06-20
IL222403A (en) 2014-08-31
KR101506776B1 (ko) 2015-03-27
CR20120513A (es) 2012-11-01
PL2560975T3 (pl) 2015-11-30
DK2560975T3 (en) 2015-06-29
US8492376B2 (en) 2013-07-23
KR20130008619A (ko) 2013-01-22
PH12012502066A1 (en) 2019-07-10
SI2560975T1 (sl) 2015-08-31
CN102858776B (zh) 2016-01-20
UA109543C2 (xx) 2015-09-10

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